WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H526771
CAS#: 1044871-04-6
Description: RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 is structurally related to the clinical compound RVX-208, currently undergoing phase III clinical trials for the treatment of cardiovascular diseases, but is distinctly different in its biological and pharmacokinetic profiles. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein. Selective inhibition of either BD1 or BD2 can have significant implications on differential gene expression, which possibly can be further linked to the specific disease indication.
Hodoodo Cat#: H526771
Name: RVX-297
CAS#: 1044871-04-6
Chemical Formula: C24H29N3O4
Exact Mass: 423.22
Molecular Weight: 423.513
Elemental Analysis: C, 68.06; H, 6.90; N, 9.92; O, 15.11
Synonym: RVX-297; RVX 297; RVX297.
IUPAC/Chemical Name: 2-(3,5-dimethyl-4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-5,7-dimethoxyquinazolin-4(3H)-one
InChi Key: PQZDYFRDRHRZGF-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H29N3O4/c1-15-11-17(12-16(2)22(15)31-10-9-27-7-5-6-8-27)23-25-19-13-18(29-3)14-20(30-4)21(19)24(28)26-23/h11-14H,5-10H2,1-4H3,(H,25,26,28)
SMILES Code: COC1=C(C(NC(C2=CC(C)=C(OCCN3CCCC3)C(C)=C2)=N4)=O)C4=CC(OC)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 423.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Kharenko OA, Gesner EM, Patel RG, Norek K, White A, Fontano E, Suto RK, Young
PR, McLure KG, Hansen HC. RVX-297- a novel BD2 selective inhibitor of BET
bromodomains. Biochem Biophys Res Commun. 2016 Aug 12;477(1):62-7. doi:
10.1016/j.bbrc.2016.06.021. Epub 2016 Jun 6. PubMed PMID: 27282480.